Pharmacology of Serotonin Receptors and Ergot Alkaloids
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Questions and Answers

What type of receptor is negatively coupled to adenylyl cyclase and primarily acts in the Raphe Nucleus?

  • 5-HT 2A
  • 5-HT 1A (correct)
  • 5-HT 1B
  • 5-HT 2C

    • Which of the following antagonists is associated with the 5-HT 2A receptor?

  • Isamaltone
  • Ketanserin (correct)
  • 5-CAT
  • Spiperone (correct)

    • Which sub-type of the 5-HT receptor is primarily expressed in the stomach and fundus?

  • 5-HT 1D
  • 5-HT 2B
  • 5-HT 1B
  • 5-HT 2C (correct)

    • What effect is primarily mediated by the 5-HT 1D receptor?

    <p>Inhibiting adenylyl cyclase</p> Signup and view all the answers

    What is the primary role of 5-HT3R antagonists?

    <p>Act as anti-emetics</p> Signup and view all the answers

    What are the primary classifications of migraine according to clinical features?

    <p>Migraine with aura</p> Signup and view all the answers

    What role do serotonin receptors 5-HT1B/D play during a migraine attack?

    <p>Inhibit vasodilation</p> Signup and view all the answers

    What triggers can induce migraine episodes?

    <p>Foods, drinks, and environmental cues</p> Signup and view all the answers

    Which of the following neuropeptides is released upon stimulation of trigeminal nerves during a migraine?

    <p>Substance P</p> Signup and view all the answers

    What type of receptor is the 5-HT3 receptor classified as?

    <p>Ligand-gated ion channel</p> Signup and view all the answers

    What characterizes ocular or retinal migraine?

    <p>Temporary blindness and blurred vision</p> Signup and view all the answers

    Which of the following is positively coupled to adenylyl cyclase?

    <p>5-HT4 receptor</p> Signup and view all the answers

    Which region in the body is associated with the 5-HT4 receptor?

    <p>Ileum</p> Signup and view all the answers

    What is the prototypical triptan drug used for migraine relief?

    <p>Sumatriptan</p> Signup and view all the answers

    What is a known effect of the 5-HT7 receptor?

    <p>Relaxation of smooth muscle</p> Signup and view all the answers

    Which mechanism is primarily involved in the maintenance of migraine pain?

    <p>Decreased inhibition of central pain transmission</p> Signup and view all the answers

    What effect do triptans have when used during a migraine attack?

    <p>Cause vasoconstriction</p> Signup and view all the answers

    Which of the following substances acts on the 5-HT6 receptor?

    <p>Clozapine</p> Signup and view all the answers

    Which receptor is associated with the action of Lisuride?

    <p>5-HT5 receptor</p> Signup and view all the answers

    What is the role of metergoline in serotonin pharmacology?

    <p>Serotonin receptor antagonist</p> Signup and view all the answers

    In which regions is the 5-HT6 receptor primarily distributed?

    <p>Thalamus and nucleus accumbens</p> Signup and view all the answers

    What is the primary distinction made between memorization and knowledge?

    <p>Knowledge involves understanding relationships between concepts.</p> Signup and view all the answers

    Which resource is recommended for literature searches?

    <p>South College Online Library</p> Signup and view all the answers

    What action is suggested if a concept does not make sense?

    <p>Contact the Faculty who taught that concept.</p> Signup and view all the answers

    What is the recommended first step before scheduling an appointment with Faculty?

    <p>Contact them via email to arrange a time.</p> Signup and view all the answers

    Which of the following is NOT listed as a resource for pharmacological studies?

    <p>Social media platforms</p> Signup and view all the answers

    Which class of agents is primarily used as 5-HT1 agonists for migraine treatment?

    <p>Triptans</p> Signup and view all the answers

    What is the primary mechanism of action (MOA) for serotonin agonists used in migraine therapy?

    <p>Agonism of serotonin receptors</p> Signup and view all the answers

    What is the consequence of relying solely on memorization according to the content?

    <p>It may only provide short-term assistance.</p> Signup and view all the answers

    Which textbook is explicitly required for coursework?

    <p>Basic &amp; Clinical Pharmacology by Katzung.</p> Signup and view all the answers

    Which of the following conditions is treated using 5-HT4 agonists?

    <p>Irritable bowel syndrome</p> Signup and view all the answers

    What adverse effect is commonly associated with the use of SSRIs?

    <p>Serotonin syndrome</p> Signup and view all the answers

    What should students do if they have persistent concerns about course material?

    <p>Contact Faculty for assistance.</p> Signup and view all the answers

    Which pharmacological class includes agents that are primarily 5-HT3 antagonists?

    <p>Anti-emetics</p> Signup and view all the answers

    Which of the following is an example of a potential drug-drug interaction (DDI) that could lead to serotonin syndrome?

    <p>MAOIs with SSRIs</p> Signup and view all the answers

    Which of the following pharmacokinetic aspects is crucial when considering the use of serotonergic agents?

    <p>Half-life and metabolism</p> Signup and view all the answers

    What is a key characteristic of ergot alkaloids in the context of migraine treatment?

    <p>They directly activate 5-HT1 receptors.</p> Signup and view all the answers

    What physiological functions are primarily regulated by 5-HT2A receptors?

    <p>Cardiovascular function and muscle contraction</p> Signup and view all the answers

    Which drug functions as both a 5-HT2A receptor antagonist and an α1/α2 irreversible blocker?

    <p>Phenoxybenzamine</p> Signup and view all the answers

    What is the primary indication for Ondansetron?

    <p>Nausea and vomiting associated with surgery and chemotherapy</p> Signup and view all the answers

    Which of the following is a boxed warning for Alosetron?

    <p>Increased risk of ischemic colitis</p> Signup and view all the answers

    What action does Tegaserod primarily facilitate in the gastrointestinal system?

    <p>Facilitating acetylcholine release for peristalsis</p> Signup and view all the answers

    Which receptor type do 5-HT3 receptors represent?

    <p>Ion channel</p> Signup and view all the answers

    Which of the following drugs is recognized for having anti-cholinergic activity along with being a 5-HT2A antagonist?

    <p>Cyproheptadine</p> Signup and view all the answers

    What distinct risk is associated with potent 5-HT4 receptor agonists?

    <p>Cardiac adverse effects</p> Signup and view all the answers

    Study Notes

    Pharmacology of Serotonin Receptor Agonists and Antagonists, and Ergot Alkaloids

    • Maha Abdalla, PharmD, PhD, RPh is an Associate Professor of Pharmaceutical Sciences at South College.
    • Office Room: 276
    • Phone: (865)288-5837
    • Office Hours: Tuesday & Thursday 9 am - 12 pm or by appointment.
    • Email: [email protected]

    Serotonin (5-hydroxytryptamine, aka 5-HT)

    • Bio synthesis & Metabolism
    • Serotonin Receptors: GPCR: 5-HT₁R, 5-HT₂R, 5-HT₄R. Na/K ion channel: 5-HT₃R
    • Migraine Management (Headache Society Consensus Statement): Update on integrating new migraine treatments into clinical practice.

    Triptans

    • Selective 5-HT₁B/D type receptor agonist
    • Sumatriptan, rizatriptan, zolmitriptan, eletriptan, almotriptan, naratriptan, frovatriptan

    Ergot Alkaloids

    • Nonselective 5-HT agonist
    • Dihydroergotamine (Migranal), Ergotamine (Ergomar)
    • CGRP Receptor Antagonist:
    • BOTH prophylaxis & acute treatment: Nurtec ODT (rimegepant) – PO
    • Ubrelvy (ubrogepant)-PO, Zavzpret (zavegepant)- Nasal spray
    • Qulipta (atogepant) – PO
    • Aimovig (erenumab-aooe)-subQ
    • Emgality (galcanezumab-gnlm), Ajovy (fremanezumab-vfrm)
    • Vyepti (Eptinezumab-jjmr)

    5-HT2 Receptor Antagonist

    • Antidepressant and Antipsychotics: Olanzapine, clozapine, Risperidone

    5-HT3 Receptor Antagonist

    • Antiemetic: Ondansetron
    • Alosetron - Restricted Use

    5-HT4 receptors partial agonists

    Serotonin Syndrome

    • Other drug classes that affect serotonin levels:
      • Selective Serotonin Reuptake Inhibitors (SSRIs): Sertraline, fluoxetine, paroxetine, citalopram, escitalopram
      • Monoamine Oxidase Inhibitors (MAOIs): Tranylcypromine, phenelzine

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    Description

    This quiz covers the pharmacology of serotonin receptor agonists and antagonists, focusing specifically on their biosynthesis, metabolism, and role in migraine management. It also includes key information about triptans and ergot alkaloids, along with the pharmacological implications of CGRP receptor antagonists in treatment. Test your knowledge on these essential topics in pharmaceutical sciences.

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